Ip Kendice, Davis Courtaney, Iqbal Zainab, McCarthy Jennifer, White Andrea, Day A J, Urwin Craig, Carvalho Maria
Research and Development (KI, MC), PCCA, Houston, TX.
Formulations (CD), PCCA, Houston, TX.
J Pediatr Pharmacol Ther. 2024 Dec;29(6):604-609. doi: 10.5863/1551-6776-29.6.604. Epub 2024 Dec 9.
In the United States, ursodiol is commercially available as solid dosage forms, which represents a problem for children who cannot swallow capsules or tablets. There is a lack of an age-appropriate formulation for ursodiol, and the extemporaneous preparation of an oral suspension with an extended beyond-use-date (BUD) may represent a good therapeutic alternative for the pediatric population. However, all pharmacists need validated stability studies to prepare oral liquids with high quality and safety.
Oral compounded suspensions for ursodiol 20 to 60 mg/mL were prepared by adding the contents of ursodiol 300-mg commercial capsules (Actavis, KVK Tech, and Mylan) to a proprietary oral suspending vehicle. The BUD of the oral compounded suspensions was determined by using a valid, stability-indicating analytical method. The physical characterization consisted of observing all samples for appearance and color, and testing for pH. Microbiological stability testing followed the United States Pharmacopeia (USP) Chapter 51: Antimicrobial Effectiveness Testing.
The ursodiol oral compounded suspensions exhibited a homogeneous white color and the pH did not change significantly. The potency of the oral suspensions remained within ±10% of the specifications. Considering the microbiological characterization, there was no growth of challenge microorganisms throughout the study for all samples.
This study demonstrates that ursodiol (Actavis, KVK Tech, and Mylan) is physically, chemically, and microbiologically stable in the oral suspending vehicle at room temperature for up to 6 months.
在美国，熊去氧胆酸有固体剂型出售，这对无法吞咽胶囊或片剂的儿童来说是个问题。熊去氧胆酸缺乏适合儿童年龄段的剂型，而临时配制超出使用期限（BUD）的口服混悬液可能是儿科患者的一个良好治疗选择。然而，所有药剂师都需要经过验证的稳定性研究来制备高质量和安全的口服液体。
通过将300毫克熊去氧胆酸商业胶囊（阿克塔维斯、KVK科技和迈兰）的内容物加入到一种专利口服混悬剂载体中，制备20至60毫克/毫升的熊去氧胆酸口服复方混悬液。通过使用有效的、稳定性指示分析方法来确定口服复方混悬液的BUD。物理特性包括观察所有样品的外观和颜色，并测试pH值。微生物稳定性测试遵循美国药典（USP）第51章：抗菌效力测试。
熊去氧胆酸口服复方混悬液呈现均匀的白色，pH值没有显著变化。口服混悬液的效价保持在规格的±10%以内。考虑到微生物特性，在整个研究过程中，所有样品的挑战微生物均未生长。
本研究表明，熊去氧胆酸（阿克塔维斯、KVK科技和迈兰）在口服混悬剂载体中于室温下在长达6个月的时间内物理、化学和微生物学性质稳定。
